- Antibacterial and antitubercular activity of novel benzothiazole- aryl amine derivatives tethered through acetamide functionality
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A novel series of substituted benzothiazole-N-phenyl acetamides were synthesized through a feasible scheme and characterized by IR, 1H NMR and mass spectral methods. All the synthesized compounds were screened for antibacterial activity against two, Gram-positive strains: Staphylococcus aureus, Bacillus subtilis; four, Gram-negative strains: Escherichia coli, Salmonella typhi, Pseudomonas aeruginosa and Klebsiella pneumonia; and antitubercular activity against mycobacterial strain: Mycobacterium tuberculosis. Among the 15 compounds (6a-o) tested, three compounds 6e, 6l and 6m have demonstrated high potency with MIC values ranges from 6.25-12.5 μg/mL against both Gram-positive and Gram-negative strains. Compounds 6e and 6l displayed remarkable antitubercular activity with MIC value of 25μg/mL.
- HAKIM, FARHANA,ROSHAN SALFIDOER
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p. 1757 - 1763
(2021/07/31)
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- An efficient synthesis of novel di-heterocyclic benzazole derivatives and evaluation of their antiproliferative activities
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A series of unsymmetrical nine di-heterocyclic compounds of benzazole derivatives were synthesized at one step via cyclization reaction. The compounds evaluated for in?vitro cytotoxic activity against A549, A498, HeLa, and HepG2 cancer cell lines. The biological evaluation results show that 23, 26 and 29 exhibit better activity against HepG2 and HeLa cancer cell lines. Compound 23 also showed good activity against A549, and A498 cancer cell lines. The analogs were further performed molecular docking studies against human cytochrome P450 2C8 monooxygenase enzyme, calculated some theoretical quantum parameters, ADMET descriptor and molecular electrostatic potential analysis. The strategy applied in this research work may act as a perspective for the rational design of potential anticancer drugs. Communicated by Ramaswamy H. Sarma.
- Algul, Oztekin,Ersan, Ronak Haj,Alagoz, Mehmet Abdullah,Duran, Nizami,Burmaoglu, Serdar
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p. 6926 - 6938
(2020/08/13)
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- Substituted amide phenol compound and its preparation method, pharmaceutical composition and use thereof
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The invention discloses substituted-amide phenolic compounds, their preparation method, a pharmaceutical composition and an application thereof. The compounds have a structure as shown in the general formula I, wherein Z, L and Q are as defined in the spe
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Paragraph 0250; 0255-0258
(2019/07/04)
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